Total synthesis of two isoflavone C-glycosides: genistein and orobol 8-C-beta-D-glucopyranosides

Carbohydr Res. 2006 Jul 3;341(9):1091-5. doi: 10.1016/j.carres.2006.03.038. Epub 2006 Apr 27.

Abstract

Genistein and orobol 8-C-beta-D-glucopyranosides (1 and 3) were firstly synthesized in overall yields of 39% and 41% from 2,4-di-O-benzylphloroacetophenone (4), as follows: (1) the formation of the chalcone (6, 7) by aldol condensation of the benzyl-protected C-glycosylphloroacetophenone (5), a key intermediate of the total synthesis of 1 and 3 and synthesized by a C-glycosylation method involving the O-->C glycoside rearrangement of 4 in 96% yield; (2) the formation of isoflavones (10, 11 and 12, 13) by the formation of acetals by oxidative rearrangement of the protected chalcones (8 and 9) using Tl(NO3)3, followed by acid-catalyzed cyclization; (3) a final debenzylation by hydrogenolysis.

MeSH terms

  • Flavonoids / chemical synthesis*
  • Genistein / chemical synthesis*
  • Glucose / analogs & derivatives*

Substances

  • Flavonoids
  • Genistein
  • Glucose
  • orobol